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RU2227022C2 - Bioadhesive buccal sustained-release tablet - Google Patents

Bioadhesive buccal sustained-release tablet

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RU2227022C2
RU2227022C2 RU2001107846/15A RU2001107846A RU2227022C2 RU 2227022 C2 RU2227022 C2 RU 2227022C2 RU 2001107846/15 A RU2001107846/15 A RU 2001107846/15A RU 2001107846 A RU2001107846 A RU 2001107846A RU 2227022 C2 RU2227022 C2 RU 2227022C2
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weight
tablet
active ingredient
amount
water
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RU2001107846/15A
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RU2001107846A (en
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Виль м Ж. БОЛОНЬЯ (FR)
Вильям Ж. БОЛОНЬЯ
Говард Л. ЛЕВАЙН (US)
Говард Л. ЛЕВАЙН
Филипп КАРТЬЕ (FR)
Филипп КАРТЬЕ
ЗЬЕГЛЕ Доминик ДЕ (FR)
ЗЬЕГЛЕ Доминик ДЕ
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Колумбия Лабораториз (Бермуда) Лимитед
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    • A—HUMAN NECESSITIES
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26—Androgens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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    • A61K9/00—Medicinal preparations characterised by special physical form
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    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
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    • A61K9/00—Medicinal preparations characterised by special physical form
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    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin

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Abstract

FIELD: medicine, pharmacy. SUBSTANCE: invention proposes bioadhesive buccal or vaginal sustained-release tablet in releasing active component for 12 h and above, in particular, testosterone, method for delivery of active component to patient blood, method for corresponding treatment, in particular, Alzheimer's disease or ischemia with testosterone, and methods for preparing bioadhesive buccal or vaginal tablet. Invention provides the composition, protection against moisture of dried core and the ratio of filling agents including polycarbophilic agent and cellulose derivative. EFFECT: expanded assortment of agents and methods for indicated designation. 27 cl, 6 dwg, 5 tbl

Description

Текст описания в факсимильном виде (см. графическую часть).Description text in facsimile form (see graphic part).

Claims (30)

1. Постепенно гидратирующаяся биоадгезивная таблетка непрерывного выделения, содержащая эффективное количество активного ингредиента, около 5-50% по массе целлюлозы, около 0,5-25% по массе крахмала, около 1-50% по массе лактозы, около 0,5-10% по массе водонерастворимого поперечно-сшитого поликарбоксильного полимера и около 1-75% по массе водорастворимого полимера.1. Gradually hydrating bioadhesive continuous release tablet containing an effective amount of the active ingredient, about 5-50% by weight of cellulose, about 0.5-25% by weight of starch, about 1-50% by weight of lactose, about 0.5-10 % by weight of a water-insoluble cross-linked polycarboxylic polymer and about 1-75% by weight of a water-soluble polymer. 2. Таблетка по п.1, отличающаяся тем, что указанная таблетка содержит вплоть до около 50% по массе активного ингредиента.2. The tablet according to claim 1, characterized in that said tablet contains up to about 50% by weight of the active ingredient. 3. Таблетка по п.2, дополнительно содержащая около 1% по массе диоксида кремния.3. The tablet according to claim 2, additionally containing about 1% by weight of silicon dioxide. 4. Таблетка по п.3, дополнительно содержащая около 0,5-2% по массе талька.4. The tablet according to claim 3, additionally containing about 0.5-2% by weight of talc. 5. Таблетка по п.4, дополнительно содержащая около 0,5-1% по массе стеарата магния.5. The tablet according to claim 4, additionally containing about 0.5-1% by weight of magnesium stearate. 6. Таблетка по п.1 или 5, отличающаяся тем, что указанный активный ингредиент выбирают из группы, состоящей из гликопротеинов, белков, половых гормонов, антигормонов, нитратов, бета-агонистов, бета-антагонистов, опиоидов, антагонистов опиоидов, антидепрессантов, ингибиторов редуктазы HMG СоА, антигистаминов, АСЕ ингибиторов, простагландинов и любого другого активного ингредиента, который подвержен метаболизму или разложению под воздействием влаги, ферментов или рН.6. The tablet according to claim 1 or 5, characterized in that said active ingredient is selected from the group consisting of glycoproteins, proteins, sex hormones, antihormones, nitrates, beta agonists, beta antagonists, opioids, opioid antagonists, antidepressants, inhibitors HMG CoA reductase, antihistamines, ACE inhibitors, prostaglandins, and any other active ingredient that is metabolized or degraded by moisture, enzymes, or pH. 7. Таблетка по п.5, отличающаяся тем, что указанный крахмал присутствует в количестве около 2-10% по массе, указанная лактоза присутствует в количестве около 8-16% по массе, указанный водорастворимый полимер присутствует в количестве около 25-35% по массе и указанная таблетка адаптирована для доставки указанного активного ингредиента в поток крови пациента через его вагинальную полость.7. The tablet according to claim 5, characterized in that said starch is present in an amount of about 2-10% by weight, said lactose is present in an amount of about 8-16% by weight, said water-soluble polymer is present in an amount of about 25-35% by weight the mass and the specified tablet is adapted for delivery of the specified active ingredient into the patient’s blood stream through his vaginal cavity. 8. Таблетка по п.5, отличающаяся тем, что указанный крахмал присутствует в количестве около 14-24% по массе, указанная лактоза присутствует в количестве около 17-27% по массе, указанный водорастворимый полимер присутствует в количестве около 5-20% по массе и указанная таблетка адаптирована для доставки указанного активного ингредиента в поток крови пациента через его буккальную полость.8. The tablet according to claim 5, characterized in that said starch is present in an amount of about 14-24% by weight, said lactose is present in an amount of about 17-27% by weight, said water-soluble polymer is present in an amount of about 5-20% by weight the mass and the specified tablet is adapted to deliver the specified active ingredient into the patient’s blood stream through its buccal cavity. 9. Постепенно гидратирующаяся биоадгезивная таблетка непрерывного выделения, содержащая эффективное количество активного ингредиента, около 2-30% по массе связующего, около 5-40% по массе лактозы, около 1-3% по массе водонерастворимого поперечно-сшитого поликарбоксильного полимера и около 5-50% по массе водорастворимого полимера.9. A gradually hydrating bioadhesive continuous release tablet containing an effective amount of the active ingredient, about 2-30% by weight of a binder, about 5-40% by weight of lactose, about 1-3% by weight of a water-insoluble crosslinked polycarboxylic polymer and about 5- 50% by weight of a water-soluble polymer. 10. Таблетка по п.9, дополнительно содержащая около 0,2-2% по массе диоксида кремния.10. The tablet according to claim 9, additionally containing about 0.2-2% by weight of silicon dioxide. 11. Буккальная таблетка по п.10, дополнительно содержащая около 0,5-2% по массе талька.11. The buccal tablet of claim 10, additionally containing about 0.5-2% by weight of talc. 12. Таблетка по п.11, дополнительно содержащая около 0,5-2% по массе стеарата магния.12. The tablet according to claim 11, additionally containing about 0.5-2% by weight of magnesium stearate. 13. Таблетка по п.11, отличающаяся тем, что указанным активным ингредиентом является тестостерон и указанный тестостерон присутствует в количестве около 1-30% по массе.13. The tablet according to claim 11, characterized in that said active ingredient is testosterone and said testosterone is present in an amount of about 1-30% by weight. 14. Таблетка по п.13, отличающаяся тем, что указанным связующим является крахмал и он присутствует в количестве около 2-10% по массе, указанная лактоза присутствует в количестве около 8-16% по массе, указанный водорастворимый полимер присутствует в количестве около 25-35% по массе и указанная таблетка адаптирована для доставки активного ингредиента в поток крови пациента через его вагинальную полость.14. The tablet according to item 13, wherein the specified binder is starch and it is present in an amount of about 2-10% by weight, the specified lactose is present in an amount of about 8-16% by weight, the specified water-soluble polymer is present in an amount of about 25 -35% by weight and the specified tablet is adapted for delivery of the active ingredient into the patient’s blood stream through his vaginal cavity. 15. Таблетка по п.13, отличающаяся тем, что указанный крахмал присутствует в количестве около 14-24% по массе, указанная лактоза присутствует в количестве около 17-27% по массе, указанный водорастворимый полимер присутствует в количестве около 5-20% по массе и указанная таблетка приспособлена для выделения указанного активного ингредиента в поток крови пациента через его буккальную полость.15. The tablet according to item 13, wherein said starch is present in an amount of about 14-24% by weight, said lactose is present in an amount of about 17-27% by weight, said water-soluble polymer is present in an amount of about 5-20% by weight the mass and the specified tablet is adapted to highlight the specified active ingredient in the patient’s blood stream through its buccal cavity. 16. Способ доставки активного ингредиента пациенту, включающий введение активного ингредиента с помощью постепенно гидратирующейся биоадгезивной таблетки непрерывного выделения, содержащей эффективное количество активного ингредиента около 5-50% по массе целлюлозы, около 0,5-25% по массе крахмала, около 1-50% по массе лактозы, около 0,5-10% по массе водонерастворимого поперечно-сшитого поликарбоксильного полимера и около 1-75% по массе водорастворимого полимера.16. A method of delivering an active ingredient to a patient, comprising administering the active ingredient using a gradually hydrating bioadhesive continuous release tablet containing an effective amount of the active ingredient of about 5-50% by weight of cellulose, about 0.5-25% by weight of starch, about 1-50 % by weight of lactose, about 0.5-10% by weight of a water-insoluble cross-linked polycarboxylic polymer and about 1-75% by weight of a water-soluble polymer. 17. Способ по п.16, отличающийся тем, что активным ингредиентом является тестостерон.17. The method according to clause 16, wherein the active ingredient is testosterone. 18. Способ лечения или профилактики ишемии или болезни Альцгеймера, включающий введение нуждающемуся в них пациенту постепенно гидратирующейся биоадгезивной таблетки непрерывного выделения, содержащей терапевтически эффективное количество тестостерона, около 5-50% по массе целлюлозы, около 0,5-25% по массе крахмала, около 1-50% по массе лактозы, около 0,5-10% по массе водонерастворимого поперечно-сшитого поликарбоксильного полимера и около 1-75% по массе водорастворимого полимера.18. A method of treating or preventing ischemia or Alzheimer's disease, comprising administering to a patient in need thereof a gradually hydrating bioadhesive continuous release tablet containing a therapeutically effective amount of testosterone, about 5-50% by weight of cellulose, about 0.5-25% by weight of starch, about 1-50% by weight of lactose, about 0.5-10% by weight of a water-insoluble cross-linked polycarboxylic polymer and about 1-75% by weight of a water-soluble polymer. 19. Способ по п.18, отличающийся тем, что биоадгезивная таблетка представляет собой буккальную таблетку.19. The method according to p. 18, wherein the bioadhesive tablet is a buccal tablet. 20. Способ по п.18, отличающийся тем, что биоадгезивная таблетка представляет собой вагинальную таблетку.20. The method according to p, characterized in that the bioadhesive tablet is a vaginal tablet. 21. Постепенно гидратирующаяся биоадгезивная таблетка непрерывного выделения для доставки активного ингредиента в поток крови пациента для лечения состояния здоровья, включающая терапевтически эффективное количество активного ингредиента, нерастворимый в воде поперечно-сшитый поликарбоксильный полимер и растворимый в воде полимер, причем указанная таблетка характеризуется тем, что внутреннее ядро таблетки сохраняется защищенным от влаги и окружающей среды и сухой запас активного ингредиента подвергается постепенной гидратации.21. A gradually hydrating bioadhesive tablet of continuous release for delivering the active ingredient to the patient’s blood stream for treating a health condition, comprising a therapeutically effective amount of the active ingredient, a water-insoluble crosslinked polycarboxylic polymer, and a water-soluble polymer, wherein said tablet is characterized by the fact that the internal The tablet core remains protected from moisture and the environment and the dry supply of the active ingredient undergoes gradual hydration. 22. Способ изготовления постепенно гидратирующейся биоадгезивной таблетки непрерывного выделения для доставки активного ингредиента в поток крови пациента для лечения состояния здоровья, причем указанная таблетка содержит терапевтически эффективное количество активного ингредиента, нерастворимый в воде поперечно-сшитый поликарбоксильный полимер и растворимый в воде полимер, внутреннее ядро этой таблетки сохраняется защищенным от влаги и окружающей среды и сухой запас активного ингредиента подвергается постепенной гидратации, где указанный способ включает приготовление смеси ингредиентов таблетки, после чего формуется и производится таблетка, и указанный способ характеризуется тем, что активный ингредиент, который может подвергнуться преждевременному метаболизму и/или деградации, добавляют соответственно на стадии приготовления смеси или формовки таблетки.22. A method of manufacturing a gradually hydrating bioadhesive tablet of continuous release to deliver the active ingredient to the patient’s blood stream for treating a health condition, said tablet containing a therapeutically effective amount of the active ingredient, a water-insoluble crosslinked polycarboxylic polymer and a water-soluble polymer, the inner core of which tablets are kept protected from moisture and the environment and the dry supply of the active ingredient undergoes gradual hydration, where said method comprises preparing a mixture of tablet ingredients, after which a tablet is molded and produced, and the method is characterized in that the active ingredient, which may undergo premature metabolism and / or degradation, is added respectively at the stage of preparation of the mixture or molding of the tablet. 23. Способ изготовления постепенно гидратирующейся биоадгезивной таблетки для непрерывного выделения активного ингредиента при лечении клинического состояния, требующего введения указанного активного ингредиента, отличающийся тем, что комбинируют эффективное количество активного ингредиента с целлюлозой в количестве около 5-50% по массе, с крахмалом в количестве около 0,5-25% по массе, с лактозой в количестве около 1-50% по массе, с водонерастворимым поперечно-сшитым поликарбоксильным полимером в количестве около 0,5-10% по массе и с водорастворимого полимера около 1-75% по массе получают гранулят, затем получают смесь для таблетки и ее таблетируют.23. A method of manufacturing a gradually hydrating bioadhesive tablet for continuous release of the active ingredient in the treatment of a clinical condition requiring the administration of the specified active ingredient, characterized in that the effective amount of the active ingredient is combined with cellulose in an amount of about 5-50% by weight, with starch in an amount of about 0.5-25% by weight, with lactose in an amount of about 1-50% by weight, with a water-insoluble cross-linked polycarboxylic polymer in an amount of about 0.5-10% by weight and with water About 1-75% by weight of polymer, granulate is obtained, then a tablet mixture is obtained and it is tabletted. 24. Способ по п.22 или 23, отличающийся тем, что активным ингредиентом является тестостерон.24. The method according to p. 22 or 23, characterized in that the active ingredient is testosterone. 25. Способ по п.24, отличающийся тем, что клиническим состоянием является ишемия или болезнь Альцгеймера.25. The method according to paragraph 24, wherein the clinical condition is ischemia or Alzheimer's disease. 26. Способ по п.24 или 25, отличающийся тем, что изготавливают буккальную биоадгезивную таблетку.26. The method according to paragraph 24 or 25, characterized in that the manufacture of a buccal bioadhesive tablet. 27. Способ по п.24 или 25, отличающийся тем, что изготавливают вагинальную биоадгезивную таблетку.27. The method according to paragraph 24 or 25, characterized in that the manufacture of a vaginal bioadhesive tablet. Приоритет по пунктам:Priority on points: 25.08.1998 по пп.24, 25 и 26;08/25/1998 according to paragraphs 24, 25 and 26; 23.08.1999 по пп.1-15, 21, 22;08/23/1999 according to claims 1-15, 21, 22; 24.08.1999 по пп.16-20, 23, 27.08.24.1999 according to claims 16-20, 23, 27.
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Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6624200B2 (en) * 1998-08-25 2003-09-23 Columbia Laboratories, Inc. Bioadhesive progressive hydration tablets
AU2005203703B2 (en) * 1998-08-25 2007-05-24 Columbia Laboratories (Bermuda) Limited Bioadhesive progressive hydration tablets
US7803392B2 (en) 2000-12-27 2010-09-28 University Of Kentucky Research Foundation pH-Sensitive mucoadhesive film-forming gels and wax-film composites suitable for topical and mucosal delivery of molecules
AU2002257430A1 (en) * 2001-05-01 2002-11-11 Mcgill University Androgen-mediated neuroprotection and uses thereof
US8425892B2 (en) * 2001-10-29 2013-04-23 Columbia Laboratories, Inc. Extended, controlled-release pharmaceutical compositions using charged polymers
US7709026B2 (en) 2001-10-29 2010-05-04 Columbia Laboratories, Inc. Low concentration of peroxide for treating or preventing vaginal infections
US20030114394A1 (en) * 2001-10-29 2003-06-19 Levine Howard L. Vaginally administered anti-dysrhythmic agents for treating pelvic pain
CN101327326A (en) * 2001-10-29 2008-12-24 哥伦比亚实验室(百慕大群岛)有限公司 Antirhythmic agents administered vaginally for the treatment of pelvic pain and infertility
US7005138B2 (en) * 2001-12-21 2006-02-28 Duramed Pharmaceuticals, Inc. Method of systematically delivering SSRIs
GB0210397D0 (en) * 2002-05-07 2002-06-12 Ferring Bv Pharmaceutical formulations
PA8578501A1 (en) * 2002-07-25 2005-02-04 Pharmacia Corp DOSAGE FORM ONCE A DAY OF PRAMIPEXOL
US20050226926A1 (en) 2002-07-25 2005-10-13 Pfizer Inc Sustained-release tablet composition of pramipexole
RU2005105945A (en) * 2002-08-02 2005-07-10 Рэнбакси Лабораториз Лимитед (In) SODIUM FOSINOPRIL TABLETS STORAGE STABLE
RU2213558C1 (en) * 2002-09-30 2003-10-10 Нестерук Владимир Викторович Antibacterial agent
AU2003285189B2 (en) * 2002-11-14 2006-07-27 Shear/Kershman Laboratories, Inc. Oral testosterone delivery system with improved sustained release
CA2514325C (en) * 2003-01-24 2013-11-12 Magle Holding Ab A composition material for transmucosal delivery
SE0302947D0 (en) 2003-01-24 2003-11-07 Magle Ab A composition material for transmucosal delivery
CA2568640C (en) 2004-06-04 2011-08-09 Teva Pharmaceutical Industries Ltd. Pharmaceutical composition containing irbesartan
DE602005024570D1 (en) * 2004-08-13 2010-12-16 Boehringer Ingelheim Pharma TABLET FORMULATION WITH EXTENDED RELEASE WITH PRAMIPEXOL OR A PHARMACEUTICALLY ALLOWED SALT, MANUFACTURING METHOD AND USE THEREOF
SG164375A1 (en) * 2004-08-13 2010-09-29 Boehringer Ingelheim Int Extended release pellet formulation containing pramipexole or a pharmaceutically acceptable salt thereof, method for manufacturing the same and use thereof
CA2610465A1 (en) * 2005-06-03 2006-12-14 Duramed Pharmaceuticals, Inc. Pharmaceutical compositions comprising prostanoid-receptor agonists and methods of making and using the same
US20070048369A1 (en) * 2005-08-26 2007-03-01 National Starch And Chemical Investment Holding Corporation Mucosal delivery tablet
WO2007070632A2 (en) 2005-12-13 2007-06-21 Biodelivery Sciences International, Inc. Abuse resistant transmucosal drug delivery device
US20090041844A1 (en) * 2006-02-10 2009-02-12 Boehringer Ingelheim International Gmbh Modified Release Formulation
WO2007090883A1 (en) * 2006-02-10 2007-08-16 Boehringer Ingelheim International Gmbh Extended release formulation
WO2007096906A2 (en) * 2006-02-27 2007-08-30 Panacea Biotec Ltd. Novel buccoadhesive compositions and process of preparation thereof
EP1837020A1 (en) 2006-03-24 2007-09-26 Bioalliance Pharma Mucosal bioadhesive slow release carrier for delivering active principles
US20070248655A1 (en) * 2006-04-21 2007-10-25 Haley Jeffrey T Lenticular shaped protective mouth sore discs
EP1872775A1 (en) * 2006-06-29 2008-01-02 Polichem S.A. Use of a hydrophilic matrix comprising a polyacrylic acid derivative, a cellulose ether and a disintegrant for the manufacture of a medicament for treating female genital disorders
SI2054031T1 (en) 2006-07-21 2016-09-30 Biodelivery Sciences International, Inc. Transmucosal delivery devices with enhanced uptake
US20100028447A1 (en) 2007-01-22 2010-02-04 Targacept, Inc. Intranasal, Buccal, And Sublingual Administration Of Metanicotine Analogs
PL2118123T3 (en) 2007-01-31 2016-06-30 Dana Farber Cancer Inst Inc Stabilized p53 peptides and uses thereof
US8828981B2 (en) 2007-02-06 2014-09-09 George Creasy Progesterone for the treatment or prevention of spontaneous preterm birth
KR101525754B1 (en) 2007-03-28 2015-06-09 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 Stitched polypeptides
EP1987820A1 (en) * 2007-05-04 2008-11-05 Christian Fiala, Ph. D. Slow release misoprostol for obstetric and/or gynaecological applications
EP2293779A1 (en) * 2008-04-24 2011-03-16 Evestra, Inc. Oral contraceptive dosage forms comprising a progestogen dispersed in an enteric polymer and further comprising an estrogen
EP2163240A1 (en) * 2008-09-12 2010-03-17 Universita' Degli Studi Di Genova A method for the production of bioadhesive compact matrices
MX343193B (en) 2009-06-18 2016-10-26 Allergan Inc Safe desmopressin administration.
CA2807685C (en) 2010-08-13 2020-10-06 Aileron Therapeutics, Inc. P53 derived peptidomimetic macrocycle
MX352959B (en) 2011-08-18 2017-12-15 Biodelivery Sciences Int Inc Abuse-resistant mucoadhesive devices for delivery of buprenorphine.
TW201806968A (en) 2011-10-18 2018-03-01 艾利倫治療公司 Peptidomimetic macrocycles
US9901539B2 (en) 2011-12-21 2018-02-27 Biodelivery Sciences International, Inc. Transmucosal drug delivery devices for use in chronic pain relief
CA2864120A1 (en) 2012-02-15 2013-08-22 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
BR112014020103A2 (en) 2012-02-15 2018-10-09 Aileron Therapeutics, Inc. peptidomimetic macrocycles
KR20150082307A (en) 2012-11-01 2015-07-15 에일러론 테라퓨틱스 인코포레이티드 Disubstituted amino acids and methods of preparation and use thereof
MX2017003797A (en) 2014-09-24 2017-06-15 Aileron Therapeutics Inc Peptidomimetic macrocycles and uses thereof.
US10253067B2 (en) 2015-03-20 2019-04-09 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
EA202192716A1 (en) 2019-04-05 2022-01-17 Гедеа Байотек Аб COMPOSITION OF THE VAGINAL TABLETS

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2108841A (en) * 1981-10-20 1983-05-25 Robert Gething Sustained release layered pharmaceutical compositions
RU2095064C1 (en) * 1995-11-24 1997-11-10 Анатолий Борисович Давыдов Agent for platelet aggregation decrease in circulatory system

Family Cites Families (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3133862A (en) 1960-07-22 1964-05-19 Miles Lab Buccal tablet containing vitamin a and sodium proteinate
GB2042888B (en) 1979-03-05 1983-09-28 Teijin Ltd Preparation for administration to the mucosa of the oral or nasal cavity
US4389393A (en) 1982-03-26 1983-06-21 Forest Laboratories, Inc. Sustained release therapeutic compositions based on high molecular weight hydroxypropylmethylcellulose
CA1208558A (en) 1982-10-07 1986-07-29 Kazuo Kigasawa Soft buccal
US5225196A (en) * 1983-11-14 1993-07-06 Columbia Laboratories, Inc. Bioadhesive compositions and methods of treatment therewith
EP0501523B1 (en) 1983-11-14 1997-04-09 Columbia Laboratories, Inc. Bioadhesive compositions
US4540566A (en) 1984-04-02 1985-09-10 Forest Laboratories, Inc. Prolonged release drug dosage forms based on modified low viscosity grade hydroxypropylmethylcellulose
JPS60215622A (en) * 1984-04-09 1985-10-29 Toyobo Co Ltd Sustained release preparation for mucosa in oral cavity
US4740365A (en) 1984-04-09 1988-04-26 Toyo Boseki Kabushiki Kaisha Sustained-release preparation applicable to mucous membrane in oral cavity
US4596795A (en) 1984-04-25 1986-06-24 The United States Of America As Represented By The Secretary, Dept. Of Health & Human Services Administration of sex hormones in the form of hydrophilic cyclodextrin derivatives
US4764378A (en) 1986-02-10 1988-08-16 Zetachron, Inc. Buccal drug dosage form
ES2039226T3 (en) 1986-12-30 1993-09-16 American Cyanamid Company PROCEDURE FOR PREPARING COMPOSITIONS CONTAINING POLYCARBOFIL.
US4915948A (en) 1987-08-31 1990-04-10 Warner-Lambert Company Tablets having improved bioadhesion to mucous membranes
US4900552A (en) 1988-03-30 1990-02-13 Watson Laboratories, Inc. Mucoadhesive buccal dosage forms
US5252334A (en) 1989-09-08 1993-10-12 Cygnus Therapeutic Systems Solid matrix system for transdermal drug delivery
US6017521A (en) * 1989-10-31 2000-01-25 Columbia Laboratories, Inc. Use of polycarboxylic acid polymers to treat vaginal infections
FI913127A7 (en) * 1989-10-31 1991-06-27 Watson Laboratories Mucoadhesive support system for therapeutic agent release
US5750134A (en) 1989-11-03 1998-05-12 Riker Laboratories, Inc. Bioadhesive composition and patch
US5750136A (en) 1989-11-03 1998-05-12 Riker Laboratories, Inc. Bioadhesive composition and patch
CA2043384A1 (en) * 1990-05-31 1991-12-01 Chin C. Hsu Bioadhesive carboxylic polymer composition and method relating thereto
FR2665357B1 (en) 1990-07-31 1995-03-31 Aiache Jean Marc PROCESS FOR THE PREPARATION OF A BIO-ADHESIVE GALENIC FORM AND GALENIC FORM THUS PREPARED.
US5102666A (en) 1990-09-11 1992-04-07 Oramed, Inc. Calcium polycarbophil controlled release composition and method
US5110605A (en) 1990-08-21 1992-05-05 Oramed, Inc. Calcium polycarbophil-alginate controlled release composition and method
US5686094A (en) 1991-04-01 1997-11-11 Theratech, Inc. Controlled release formulations for the treatment of xerostomia
JP2609022B2 (en) 1990-11-29 1997-05-14 北陸製薬株式会社 Polycarbophil calcium-containing preparation
JPH06100466A (en) 1992-02-14 1994-04-12 Tsumura & Co Protective agent for stress-induced neurological disorders
DK0641192T3 (en) 1992-05-18 1998-03-02 Minnesota Mining & Mfg Transmucosal drug delivery device
GR1002418B (en) * 1992-07-29 1996-08-21 Johnson & Johnson Consumer Products Inc. Bioactive treatment compositions and methods of use.
US5458884A (en) 1992-09-10 1995-10-17 Britton; Peter Bioerodible device for administering active ingredients
FI933979A0 (en) 1992-09-10 1993-09-10 Mcneil Ppc Inc BIOERODERBAR ANORDNING FOER DOSERING AV AKTIVA INGREDIENSER
US5298017A (en) 1992-12-29 1994-03-29 Alza Corporation Layered electrotransport drug delivery system
US5460820B1 (en) 1993-08-03 1999-08-03 Theratech Inc Method for providing testosterone and optionally estrogen replacement therapy to women
US5543150A (en) * 1993-09-15 1996-08-06 Columbia Laboratories, Inc. Method of progesterone delivery and affect thereof
FR2712807B1 (en) * 1993-11-24 1996-02-23 Vetoquinol Sa Solid mucoadhesive, therapeutic or hygienic composition, for administration by application to the oral or nasal mucosa.
US5578315A (en) * 1993-12-01 1996-11-26 Rutgers, The State University Of New Jersey Mucosal adhesive device for long-acting delivery of pharmaceutical combinations in oral cavity
US5567439A (en) 1994-06-14 1996-10-22 Fuisz Technologies Ltd. Delivery of controlled-release systems(s)
US5958458A (en) * 1994-06-15 1999-09-28 Dumex-Alpharma A/S Pharmaceutical multiple unit particulate formulation in the form of coated cores
AU692565B2 (en) 1994-06-16 1998-06-11 Pharmacia & Upjohn S.P.A. Bioadhesive starches and process for their preparation
US5554380A (en) 1994-08-04 1996-09-10 Kv Pharmaceutical Company Bioadhesive pharmaceutical delivery system
US5656284A (en) 1995-04-24 1997-08-12 Balkin; Michael S. Oral transmucosal delivery tablet and method of making it
US5624677A (en) 1995-06-13 1997-04-29 Pentech Pharmaceuticals, Inc. Controlled release of drugs delivered by sublingual or buccal administration
US5766620A (en) 1995-10-23 1998-06-16 Theratech, Inc. Buccal delivery of glucagon-like insulinotropic peptides
US5783212A (en) 1996-02-02 1998-07-21 Temple University--of the Commonwealth System of Higher Education Controlled release drug delivery system
DE19619045C1 (en) 1996-05-02 1997-11-13 Jenapharm Gmbh Use of combination products for the treatment of hypogonadal men and men with pituitary disorders
US5783208A (en) 1996-07-19 1998-07-21 Theratech, Inc. Transdermal drug delivery matrix for coadministering estradiol and another steroid
US5800832A (en) 1996-10-18 1998-09-01 Virotex Corporation Bioerodable film for delivery of pharmaceutical compounds to mucosal surfaces
US5807575A (en) 1997-02-14 1998-09-15 Rougier Inc. Manufacture of cross-linked amylose useful as a excipient for control release of active compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2108841A (en) * 1981-10-20 1983-05-25 Robert Gething Sustained release layered pharmaceutical compositions
RU2095064C1 (en) * 1995-11-24 1997-11-10 Анатолий Борисович Давыдов Agent for platelet aggregation decrease in circulatory system

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Технология лекарственных форм. /Под ред. Л.А.Ивановой. - М.: Медицина, 1991, т.2, с.136, 139 и 140. *

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